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Literature summary for 2.7.7.19 extracted from

  • Chen, L.S.; Sheppard, T.L.
    Chain termination and inhibition of Saccharomyces cerevisiae poly(A) polymerase by C-8-modified ATP analogs (2004), J. Biol. Chem., 279, 40405-40411.
    View publication on PubMed

Application

Application Comment Organism
drug development polyadenylation inhibition represents one mode of action for 8-chloroadenosine and 8-aminoadenosine in hematological malignancies, among several possible mechanisms. RNA-directed drugs may offer a valuable strategy in targeting indolent cancers, such as multiple myeloma Saccharomyces cerevisiae

Inhibitors

Inhibitors Comment Organism Structure
3'-dATP
-
Saccharomyces cerevisiae
8-amino-ATP C-8 substitution influences sugar pucker conformation, which may affect yPAP efficiently Saccharomyces cerevisiae
8-aza-ATP slight inhibition Saccharomyces cerevisiae
8-azido-ATP slight inhibition Saccharomyces cerevisiae
8-bromo-ATP halogen modification at C-8 may negatively affect the ability of the enzyme to activate the ATP substrate or to transfer the AMP group from the enzyme to the RNA substrate Saccharomyces cerevisiae
8-chloro-ATP
-
Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + RNAn
-
Saccharomyces cerevisiae diphosphate + RNAn+1
-
?

Synonyms

Synonyms Comment Organism
poly(A) polymerase
-
Saccharomyces cerevisiae
yPAP
-
Saccharomyces cerevisiae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0019
-
8-amino-ATP incubation at 37 °C for 20 min Saccharomyces cerevisiae
0.0063
-
3'-dATP incubation at 37 °C for 20 min Saccharomyces cerevisiae